meclinertant [Ligand Id: 1582] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL506981 (Meclinertant, SR-48692, Reminertant)
  • NTS1 receptor/Neurotensin receptor 1 in Human [ChEMBL: CHEMBL4123] [GtoPdb: 309] [UniProtKB: P30989]
  • NTS1 receptor/Neurotensin receptor 1 in Rat [ChEMBL: CHEMBL3027] [GtoPdb: 309] [UniProtKB: P20789]
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  • NTS2 receptor/Neurotensin receptor 2 in Human [ChEMBL: CHEMBL2514] [GtoPdb: 310] [UniProtKB: O95665]
  • NTS2 receptor in Mouse [GtoPdb: 310] [UniProtKB: P70310]
  • NTS2 receptor/Neurotensin receptor 2 in Rat [ChEMBL: CHEMBL5106] [GtoPdb: 310] [UniProtKB: Q63384]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
NTS1 receptor/Neurotensin receptor 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4123] [GtoPdb: 309] [UniProtKB: P30989]
ChEMBL Displacement of [3H]SR48692 from human NTR1 extracellular loop 1 F136A mutant expressed in HEK293 cells B 7.48 pKd 33 nM Kd Bioorg. Med. Chem. (2008) 16: 9359-9368 [PMID:18809332]
ChEMBL Displacement of [3H]SR48692 from human NTR1 extracellular loop 1 W129A mutant expressed in HEK293 cells B 7.57 pKd 27 nM Kd Bioorg. Med. Chem. (2008) 16: 9359-9368 [PMID:18809332]
ChEMBL Displacement of [3H]SR48692 from human NTR1 extracellular loop 1 W134A mutant expressed in HEK293 cells B 7.64 pKd 23 nM Kd Bioorg. Med. Chem. (2008) 16: 9359-9368 [PMID:18809332]
ChEMBL Displacement of [3H]SR48692 from human NTR1 extracellular loop 1 F127A mutant expressed in HEK293 cells B 7.72 pKd 19 nM Kd Bioorg. Med. Chem. (2008) 16: 9359-9368 [PMID:18809332]
ChEMBL Displacement of [3H]SR48692 from human NTR1 extracellular loop 1 P133A mutant expressed in HEK293 cells B 8.04 pKd 9.2 nM Kd Bioorg. Med. Chem. (2008) 16: 9359-9368 [PMID:18809332]
ChEMBL Displacement of [3H]SR48692 from wild type human NTR1 expressed in HEK293 cells B 8.05 pKd 8.9 nM Kd Bioorg. Med. Chem. (2008) 16: 9359-9368 [PMID:18809332]
ChEMBL Displacement of [3H]SR48692 from human NTR1 extracellular loop 1 H131A mutant expressed in HEK293 cells B 8.08 pKd 8.4 nM Kd Bioorg. Med. Chem. (2008) 16: 9359-9368 [PMID:18809332]
GtoPdb - - 8.4 pKi - - - Mol. Pharmacol. (2001) 60: 1392-8 [PMID:11723247]
ChEMBL Antagonist activity at NTSR1 (unknown origin) expressed in CHO cells assessed as inhibition of NT(8-13) peptide-induced change in intracellular Ca2+ level preincubated for 45 mins by FLIPR assay B 7.09 pIC50 82 nM IC50 Bioorg. Med. Chem. Lett. (2014) 24: 3974-3978 [PMID:24997685]
GtoPdb - - 8.2 pIC50 6.31 nM IC50 J. Pharmacol. Exp. Ther. (1997) 280: 802-12 [PMID:9023294]
ChEMBL Displacement of [125I]I-Tyr(3)NT from human NTR1 B 9 pIC50 0.99 nM IC50 J. Med. Chem. (2009) 52: 1803-1813 [PMID:19290594]
ChEMBL Agonist activity at NTR1 in human U2OS cells after 1 hr by beta-arrestin GFP reporter gene assay B 4.51 pEC50 31000 nM EC50 Bioorg. Med. Chem. Lett. (2014) 24: 262-267 [PMID:24332089]
NTS1 receptor/Neurotensin receptor 1 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3027] [GtoPdb: 309] [UniProtKB: P20789]
ChEMBL Displacement of [125I]NT from rat NTR1 transfected in mouse LTK cells B 8.59 pKi 2.6 nM Ki Bioorg. Med. Chem. (2013) 21: 4378-4387 [PMID:23721919]
GtoPdb - - 8.6 pKi - - - Mol. Pharmacol. (1995) 47: 1050-6 [PMID:7746272];
J. Biol. Chem. (1998) 273: 16351-7 [PMID:9632698]
NTS2 receptor/Neurotensin receptor 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2514] [GtoPdb: 310] [UniProtKB: O95665]
ChEMBL Binding affinity to NTR2 (unknown origin) B 6.38 pKi 418 nM Ki Bioorg. Med. Chem. (2013) 21: 4378-4387 [PMID:23721919]
GtoPdb - - 6.4 pKi - - - Mol. Pharmacol. (2001) 60: 1392-8 [PMID:11723247]
NTS2 receptor in Mouse [GtoPdb: 310] [UniProtKB: P70310]
GtoPdb - - 7.1 pIC50 - - - Biochem. Biophys. Res. Commun. (1998) 243: 585-90 [PMID:9480852]
NTS2 receptor/Neurotensin receptor 2 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5106] [GtoPdb: 310] [UniProtKB: Q63384]
ChEMBL Displacement of [125I]NT at rat NTS2 overexpressed in CHOK1 cells after 30 mins by gamma counting B 7.21 pKi 62 nM Ki J. Med. Chem. (2014) 57: 5318-5332 [PMID:24856674]
ChEMBL Agonist activity at rat NTS2 stably expressed in CHOK1 cells assessed as induction of calcium release by FLIPR assay F 6.92 pEC50 120 nM EC50 J. Med. Chem. (2014) 57: 5318-5332 [PMID:24856674]
Neurotensin receptor 3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3091] [UniProtKB: Q99523]
ChEMBL Binding affinity to NTR3 (unknown origin) B 6.62 pIC50 238 nM IC50 Bioorg. Med. Chem. (2013) 21: 4378-4387 [PMID:23721919]

ChEMBL data shown on this page come from version 26:

Gaulton A, Hersey A, Nowotka M, Bento AP, Chambers J, Mendez D, Mutowo P, Atkinson F, Bellis LJ, CibriƔn-Uhalte E, Davies M, Dedman N, Karlsson A, MagariƱos MP, Overington JP, Papadatos G, Smit I, Leach AR. (2017) 'The ChEMBL database in 2017.' Nucleic Acids Res., 45(D1). DOI: 10.1093/nar/gkw1074. [PMCID:5210557]